7Et-11F-CPT
7Et-11F-CPT is a Topoisomerase I inhibitor and an analog of 11F-CPT (HY-190897). 7Et-11F-CPT stabilizes the TOP I‑DNA cleavage complex in a non-covalent manner, promotes TOP I-related DNA damage, and activates the ATR-CHK1 DNA damage response. 7Et-11F-CPT induces cell cycle arrest predominantly in S phase accompanied by G2/M phase, upregulates Bax, Bad, and cleaved caspase‑3, and downregulates Bcl‑2, thereby inducing tumor cell apoptosis. 7Et-11F-CPT inhibits tumor growth in the PAN02 pancreatic cancer xenograft model. 7Et-11F-CPT can be used for research on pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 124622-78-2
- Formula: C22H19FN2O4
- Molecular Weight:394.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Topoisomerase I |
Caspase 3 |
Bax |
bad |
Bcl-2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
0.152 μM
|
Antiproliferative activity against human HepG2 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human HepG2 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| A549 | IC50 |
0.020 μM
|
Antiproliferative activity against human A549 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human A549 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| MCF7 | IC50 |
0.102 μM
|
Antiproliferative activity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| SW480 | IC50 |
0.045 μM
|
Antiproliferative activity against human SW480 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human SW480 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| T-24 | IC50 |
0.005 μM
|
Antiproliferative activity against human T24 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human T24 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| UMUC3 | IC50 |
0.001 μM
|
Antiproliferative activity against human UMUC3 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human UMUC3 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| PANC-1 | IC50 |
0.087 μM
|
Antiproliferative activity against human PANC-1 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human PANC-1 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| BXPC-3 | IC50 |
0.0002 μM
|
Antiproliferative activity against human BxPC-3 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human BxPC-3 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| L02 | IC50 |
0.021 μM
|
Cytotoxicity against human L02 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Cytotoxicity against human L02 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
In Vitro
7Et-11F-CPT (0.01-0.25 μM in BxPC-3; 0.1-2.5 μM in PANC-1; 24 h-14 days) inhibits BxPC-3 and PANC-1 cell proliferation in the EdU incorporation assay and inhibits long-term colony formation[1].
7Et-11F-CPT (48 h) induces γ-H2AX-positive DNA damage in BxPC-3 cells at 0.01 μM and in PANC-1 cells at 0.1 μM[1].
7Et-11F-CPT induces DNA damage and activates ATR-CHK1 signaling[1].
7Et-11F-CPT binds to TOP I in BxPC-3 cells and increases its thermal stability, promoting the trapping of TOP I on DNA in BxPC-3 cells[1].
7Et-11F-CPT (0.5 μM in BxPC-3; 2.5 μM in PANC-1) inhibits cellular TOP I activity in BxPC-3 and PANC-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC-3 and PANC-1 cells
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Concentration:BxPC-3: 0.01, 0.05, 0.25 μM; PANC-1: 0.1, 0.5, 2.5 μM
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Incubation Time:24 h (EdU)
14 days (colony) -
Result:Inhibited the proliferation of BxPC-3 and PANC-1 cells—as demonstrated in EdU incorporation assays—and suppresses long-term colony formation.
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Cell Line:BxPC-3 and PANC-1 cells
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Concentration:BxPC-3: 0.01, 0.05, 0.25 μM; PANC-1: 0.1, 0.5, 2.5 μM
-
Incubation Time:24 h
-
Result:Induced S-phase accumulation in BxPC-3 and PANC-1 cells, with S-phase fractions reaching 90.0% in BxPC-3 at 0.25 μM and 76.7% in PANC-1 at 0.1 μM.
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Cell Line:BxPC-3 and PANC-1 cells
-
Concentration:BxPC-3: 0.01, 0.05, 0.25 μM; PANC-1: 0.1, 0.5, 2.5 μM
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Incubation Time:24 h
-
Result:Increased p53 and p21 expression, increased S-phase-related CCNA1 and G2/M-related CCNB1 expression.
Decreased G1-phase-related CCND1 and CCNE1 expression in a dose-dependent manner in both cell lines.
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Cell Line:BxPC-3 and PANC-1 cells
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Concentration:BxPC-3: 0.01, 0.05, 0.25 μM; PANC-1: 0.1, 0.5, 2.5 μM
-
Incubation Time:48 h
-
Result:Induced apoptosis in BxPC-3 and PANC-1 cells in a dose-dependent manner, reaching 61.4% total apoptosis in BxPC-3 at 0.25 μM.
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Cell Line:BxPC-3 and PANC-1 cells
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Concentration:BxPC-3: 0.01, 0.05, 0.25 μM; PANC-1: 0.1, 0.5, 2.5 μM
-
Incubation Time:48 h
-
Result:Increased pro-apoptotic Bad, Bax, and cleaved caspase-3 expression and decreased anti-apoptotic Bcl-2 expression in a dose-dependent manner in both cell lines.
Increased γ-H2AX protein expression in both BxPC-3 and PANC-1 cells.
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Cell Line:BxPC-3 and PANC-1 cells
-
Concentration:BxPC-3: 0.01 μM; PANC-1: 0.1 μM
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Incubation Time:48 h
-
Result:Substantially increased the proportion of γ-H2AX-positive cells in BxPC-3 and PANC-1 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (female, 2 × 106 PAN02 cells in 150 μL)[1]
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Dosage:1.5 mg/kg and 4.5 mg/kg
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Administration:intraperitoneal; every other day; seven doses over 14 days
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Result:Suppressed PAN02 syngeneic tumor growth in mice, with tumor growth inhibition of 69.25% at 1.5 mg/kg and 80.78% at 4.5 mg/kg.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Genotoxicity/Mutagenicity Study
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 124622-78-2
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Molecular Weight 394.40
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Formula C22H19FN2O4
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SMILES
O=C1C2=C([C@](CC)(O)C(OC2)=O)C=C3C4=NC5=CC(F)=CC=C5C(CC)=C4CN31
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)